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Identification and Pharmacokinetics of Quinone Reductase 2 Inhibitors after Oral Administration of Garcinia mangostanaL. Extract in Rat by LC–MS/MS

Authors :
Liang, Xiao
Hu, Yu
Li, Jianxin
Chang, Alan K.
Tao, Xia
Li, Yanan
Liu, Wenbao
Pi, Kexin
Yuan, Jie
Jiang, Zhen
Source :
Journal of Agricultural and Food Chemistry; October 2020, Vol. 68 Issue: 43 p11975-11986, 12p
Publication Year :
2020

Abstract

Garcinia mangostanaL. (mangosteen) is a famous tropical fruit that contains a large number of xanthones. Regular consumption of mangosteen may confer health benefits and prevent some diseases, such as malaria. Quinone reductase 2 (QR-2) is a cytosolic enzyme found in human red blood cells, and it is becoming a target for chemoprevention because it is involved in the mechanisms of several diseases, including malaria. To understand whether the xanthones present in mangosteen might inhibit the activity of QR-2, blood samples were collected from rat following the oral administration of mangosteen extract and then incubated with QR-2 followed by UF–HPLC–QTOF/MS analysis to rapidly screen for and identify the QR-2-inhibiting xanthones. A total of 16 xanthones were identified, and six of these (α-mangostin, γ-mangostin, 8-deoxyartanin, 1,3,7-trihydroxy-2,8-di(3-methylbut-2-enyl)xanthone, garcinone E, and 9-hydroxycalabaxanthone) were subjected to QR-2 inhibition assay. γ-Mangostin exhibited the strongest inhibition, achieving an IC50value of 3.82 ± 0.51 μM. Its interaction with QR-2 was found to involve hydrogen bond and arene–arene interaction as revealed by molecular docking. The present study could provide new insight into the potential application of mangosteen as functional food ingredients for inhibiting the activity of QR-2. However, the extent of daily intake of mangosteen required and the exact contribution of mangosteen to the prevention and treatment of malaria remain subjects of further study.

Details

Language :
English
ISSN :
00218561 and 15205118
Volume :
68
Issue :
43
Database :
Supplemental Index
Journal :
Journal of Agricultural and Food Chemistry
Publication Type :
Periodical
Accession number :
ejs54408248
Full Text :
https://doi.org/10.1021/acs.jafc.0c04439